57 results about "Azepindole" patented technology

The invention discloses a symmetric azaindole-heptamethine cyanine J-aggregate as well as a preparation method and application thereof, and aims to solve the problems of short absorption wavelength, poor stability and the like in the prior art. The cyanine J-aggregate has the maximum absorption wavelength as long as 1035 nm, is located in an NIR-II region and has excellent photo-thermal performance and stability, and the photo-thermal stability is improved by nearly 68% compared with that of an existing J-aggregate. The preparation method comprises multiple steps of reaction, and finally self-assembly is carried out in a PBS solution to form the J-aggregate. The cyanine J-aggregate shows the capabilities of efficiently killing tumor cells and completely ablating tumors in vivo in tumor photothermal therapy, is good in biocompatibility, expands the application scene of diagnosis and treatment integration, and has a wide prospect in the field of tumor photothermal therapy.

This invention belongs to the field of pharmaceutical technology, specifically relating to a quinazoline-azaindole compound, its preparation method, and its application in treating Alzheimer's disease. The quinazoline-azaindole compound of this invention regulates NF-κB by inhibiting DYRK1A. k B. A series of signaling pathways, including PI3k-Akt, achieve anti-neuroinflammatory effects; quinazoline-azaindole compounds can reduce the expression of inflammatory factor-related genes in an LPS-induced BV2 microglial inflammation model, thereby reducing the levels of inflammatory factors in the hippocampus and cortex, alleviating neuronal pathological damage caused by neuroinflammation, and improving cognitive impairment caused by neuroinflammation; in summary, quinazoline compounds inhibit DYRK1A and downregulate NF-κB signaling pathways. k It can reduce the expression and release of inflammatory factors, improve brain tissue pathology, and alleviate cognitive impairment through signaling pathways such as B, and has significant clinical application value.

The invention discloses a 7-azaindole compound as well as a preparation method and application thereof, belongs to the field of medicine synthesis, and particularly relates to a pyrazole or indole substituted 7-azaindole compound as shown in a general formula (I) as well as a preparation method and application thereof in medicine. According to the compound disclosed by the invention, tumor cachexia skeletal muscle atrophy is relieved by inhibiting ActRIIB protein in an MSTN pathway, and a remarkable tumor cachexia resisting effect is achieved. Experimental results show that the compound has good anti-cachexia activity and can be further used for preparing novel anti-cachexia drugs. # imgabs0 #

This invention discloses a method for synthesizing a venetum intermediate, specifically as follows: Step 1: In an organic solvent, 2,4-difluorobenzoic acid and 5-hydroxy-7-azaindole undergo an etherification reaction under the action of an acid-binding agent. After the reaction, post-treatment yields 2-((1h-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-fluorobenzoic acid; Step 2: 2-((1h-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-fluorobenzoic acid reacts with 1-((2-(4-chlorophenyl)-4,4-dimethylcyclohexene-1-)methyl)piperazine in… An amination reaction occurs under the action of a base. After the reaction, post-treatment yields 2-(7-azaindole-5-oxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohexene-1-)methyl)piperazine-1-)benzoic acid, i.e., Venetantora intermediate III. The synthetic process provided by this invention avoids Grignard reactions and subsequent hydrolysis reactions, shortens the operation steps, simplifies the synthetic process, and provides a simple and easy-to-operate synthetic process. The raw materials are inexpensive and readily available, while avoiding the use of highly toxic raw materials. The production process is green and environmentally friendly, and suitable for industrial production.

The present invention concerns a compound of formula (I):or one of its pharmaceutically acceptable salts, especially for use as inhibitors of the ERK kinase activity, in particular ERK2 activity.

The present disclosure relates to compounds and compositions for inhibiting Bcr-Abl tyrosine kinase, methods for preparing the compounds and compositions, and the use of the compounds and compositions in treating various cancers such as chronic myeloid leukemia (CML).

The present invention provides compounds that inhibit rho-associated protein kinase (ROCK) for therapeutic uses as further described herein.

The present invention discloses 7-azaindole compounds, their preparation methods, and their uses, which belong to the field of drug synthesis. The present invention particularly relates to 7-azaindole compounds containing pyrazole or indole substitutions represented by general formula (I), as well as their preparation methods and pharmaceutical uses. The compounds of the present invention alleviate cancer cachexia skeletal muscle atrophy by inhibiting the ActRIIB protein in the MSTN pathway, thereby achieving significant anti-cancer cachexia effects. Experimental results show that the compounds have good anti-cachexia activity and can therefore be further used to prepare novel anti-cachexia drugs. TIFF2025537427000068.tif3144

The invention relates to the technical field of biological medicines, and particularly discloses an azaindole compound as well as a preparation method and application thereof. The azaindole compound provided by the invention is a compound as shown in a general formula I or pharmaceutically acceptable salt, isomer, solvate, hydrate, prodrug or isotope derivative of the compound, the structural formula of the general formula I is shown in the specification. The azaindole compound provided by the invention shows good inhibitory activity on BCR-ABL-T315I and BCR-ABL-WT transfected Ba / F3 cells, so that the azaindole compound can be used as a BCR-ABL inhibitor and is expected to be developed into a medicine for treating and / or preventing BCR-ABL related diseases.

The present application relates to the technical field of biological medicines, and particularly discloses an azaindole compound, a preparation method therefor, and a use thereof. The azaindole compound provided by the present application is a compound represented by general formula I or a pharmaceutically acceptable salt, an isomer, a solvate, a hydrate, a prodrug or an isotope derivative thereof; and the structural formula of general formula I is: formula I. The azaindole compound provided by the present application exhibits good inhibitory activity against Ba / F3 cells transfected with BCR-ABL-T315I and BCR-ABL-WT. Therefore, the azaindole compound can be used as a BCR-ABL inhibitor, and is expected to be developed into a drug for treating and / or preventing BCR-ABL related diseases.

This invention discloses a class of indole derivatives containing or without heteroatoms (such as nitrogen heteroatoms) and their pharmaceutical compositions that can be used as PI3Kδ kinase inhibitors, and can be used to treat diseases, conditions or symptoms related to PI3Kδ inhibition, including immune disorders, cancer and cardiovascular diseases.

This invention provides rho-associated protein kinase (ROCK) inhibiting compounds for therapeutic applications as described further herein.

This disclosure relates to solid forms of (2S)-2-[(10S,17E)-16-ethoxy-6,8,10,12,20-pentamethyl-2,8,10,11,12,13-hexahydro-14H-5,3-(azenometheno)tripyrazolo[3,4-f:3',4'-j:4'',3''-n][1,4]oxazacyclopentadecin-14-yl]propan-1-ol that are useful in the treatment of disease, such as cancer, in mammals. This disclosure also relates to the preparation of such solid forms, including polymorphs, salts, cocrystals, solvates, hydrates, or a combination thereof. This disclosure also relates to compositions including such solid forms, and to methods of using such compositions in the treatment of diseases, such as cancer, in mammals, especially in humans.

Disclosed in the present invention are 7-azaindole compounds, a preparation method therefor, and the use thereof, belonging to the field of drug synthesis. The present invention particularly relates to 7-azaindole compounds containing pyrazole or indole substitution represented by general formula (I), a preparation method therefor and the use thereof in medicine. The compounds of the present invention alleviate cancer cachexia skeletal muscle atrophy by means of inhibiting ActRIIB protein in the MSTN pathway, thereby achieving a remarkable anti-cancer-cachexia effect. Experimental results show that the compounds have good anti-cachexia activity and thus can be further used for preparing novel anti-cachexia drugs.

The invention discloses a 7-azaindole compound as shown in a formula I, an optical isomer or pharmaceutically acceptable salt thereof, and also provides a preparation method and application thereof, and the obtained compound shows a certain Menin protein expression down-regulation effect, better cell proliferation inhibition activity and better PK effect.

The disclosure generally relates to compounds of Formula I, comprising a 1,6,7,8-tetrahydro-5H-imidazo[4,5-g][1,6]isoquinolin-5-one moiety directly bonded to an azaindole or indole moiety, such compounds as inhibitors of PAD4, methods for preparing these compounds pharmaceutical compositions comprising these compounds and uses of these compounds in the treatment of a disease or a disorder associated with PAD4 enzyme activity.

The invention relates to an azaindole compound as well as a preparation method and application thereof, and belongs to the field of medicines. The invention provides a compound shown in a general formula I or a pharmaceutically acceptable salt thereof. The azaindole compound provided by the invention has a novel chemical structure, most of the compounds have high-level inhibitory activity on TNIK in vitro, and the inhibitory activity of most of the compounds on TNIK is superior to that of the disclosed compounds and a TNIK inhibitor INS018055 entering a clinical II stage at present. The compound can be used for preventing and / or treating various diseases such as cancers, nervous system diseases, fibrotic diseases or metabolic diseases, and has a very wide application prospect.

Hallucinogenic and non-hallucinogenic serotonin receptor agonists are disclosed herein in addition to methods of making and using the same.

This disclosure relates to the field of anticancer drug technology, and discloses a 7-azaindole compound, its synthesis method, and its uses. The structure of the 7-azaindole compound is as follows: This 7-azaindole compound can be used as a fluorescent polarization probe or a degradation chemical probe targeting CSN5; wherein, the fluorescent polarization chemical probe has a good binding affinity to the metalloproteinase CSN5, laying an important foundation for the discovery of novel CSN5 inhibitors; at the same time, the degradation chemical probe exhibits good enzyme-level activity and cell-inhibitory activity, and has the potential to degrade CSN5 protein and its variants, providing a material basis for the development of related drugs targeting CSN5 and the study of its biological functions, and also has great potential in the discovery of cancer immunotherapy drugs and the treatment of other related diseases.

Provided herein are compounds, including compounds of any of the formulae described herein (e.g., Formula (I)), and pharmaceutically acceptable salts, stereoisomers, tautomers, solvates, hydrates, isotopically labeled derivatives, and prodrugs thereof. Compounds provided herein can act as potentiators of voltage-gates potassium channels (e.g., Kv7 potassium channels such as Kv7.2 / Kv7.3) and are therefore useful in the treatment and / or prevention of diseases, disorders, and conditions (e.g., diseases, disorders, and conditions associated with Kv7 potassium channel dysfunction).

The invention relates to the technical field of biological detection and fluorescence labeling, and particularly discloses an alkynyl-substituted azaindole polymethine cyanine dye and a synthesis method and application thereof, the alkynyl-substituted azaindole polymethine cyanine dye has a structure as shown in the following general formula I: in the general formula I, X is selected from H, F, Cl, Br or I; y is a C or N atom; n is an integer of 0, 1 or 2; r1, R3, R5 and R6 are respectively and independently selected from hydrogen, C-Calkyl, C-Ccarboxy alkyl, aryl, aryl carboxylic ester, C-Calkyl sulfonate, aryl sulfonate, C-Calkyl sulfonamide or aryl sulfonamide; r2 and R4 are respectively and independently selected from hydrogen, halogen,-COOH,-NHH,-SOH,-SONHH, C-Calkyl carboxylic ester, C-Camino alkyl, aryl, aryl carboxylic ester, C-Calkyl sulfonate, aryl sulfonate, C-Calkyl sulfonamide or aryl sulfonamide.

The application discloses a kind of chiral 7-azaindoline amide compounds, its synthesis method and application, belong to organic chemistry synthesis and medical technology field, the compound has with N-[3-phenyl-3-(diphenyl phosphoryl) propionyl] Substituted 7-azaindoline as basic skeleton Structural characteristics;Its synthesis method is: under room temperature condition, copper salt is dissolved in organic solvent with chiral ligand (L) Stirring mixing, then sequentially adding α, β-unsaturated 7-azaindoline amide (I), diphenyl phosphine (II) And base, after stirring reaction, the target product is obtained by separation and purification;The compound provided by the application can be efficiently converted into other novel 7-azaindoline derivatives by simple reaction, and has potential application value in the field of medicinal chemistry and asymmetric catalysis;The synthesis method provided by the application has the advantages of simple operation, mild reaction condition, wide substrate applicability, high yield and high enantioselectivity.

The application discloses a 7-azaindole photoacoustic imaging probe for detecting superoxide anion, a preparation method and application, and the photoacoustic imaging probe is named AIH-OTF, which is a blue-green solid prepared from methyl trifluoromethanesulfonate, dye AIH-OH and the like; the AIH-OTF realizes high-contrast PA imaging of endogenous superoxide anion in living cells, and in-situ evaluation of occurrence and repair of acetaminophen-induced liver injury is also determined through non-invasive monitoring of the PA reaction of AIH-OTF to superoxide anion; the AIH-OTF probe can be used as a useful tool for accurately diagnosing drug-induced liver injury in vivo. The photoacoustic imaging probe can realize real-time detection of in-vivo superoxide anion through AIH-OTF and the ability of diagnosing DILI; the cell toxicity is small, the biological compatibility is good, and the photoacoustic imaging probe can be used for in-vivo imaging of occurrence and repair of DILI.

The invention provides a method for preparing kasatinib, a novel intermediate used in the method and application of the novel intermediate, and belongs to the field of medicine preparation. According to the method for preparing the kasatinib, a protecting group is introduced to a key starting material azaindole ring (pyrrolopyrimidine) for synthesizing the kasatinib, the protecting group is selected from p-toluenesulfonyl (Tos), t-butyloxycarboryl (Boc) and (trimethylsilyl) ethoxymethyl (SEM), the reaction yield is increased, the total yield reaches 58.4%, and the material cost is reduced.

This invention relates to the fields of organic light-emitting materials and tumor drugs, and particularly to a benzozaindolone compound, its preparation method, and its application. The structural formula of the benzozaindolone compound is shown in formula (3). This invention adopts a one-step synthesis strategy, which is simple, mild, has inexpensive and widely available substrates, and has a high conversion yield. It provides a simple and green synthetic approach for the synthesis of benzozaindolone compounds. Furthermore, the target compound (benzozaindolone compound) has excellent fluorescence luminescence properties and biocompatibility, and can be directly applied to fluorescence imaging of cancer cells and type I photodynamic therapy.

The present disclosure relates to compounds and compositions for inhibition of Bcr-Abl tyrosine kinases, methods of preparing said compounds and compositions, and their use in the treatment of various cancers, such as chronic myeloid leukemia (CML).

The invention discloses a green and efficient synthesis method of high-purity 4-chloro-5-fluoro-7-azaindole, which comprises the following steps: by taking 5-fluoro-1H-pyrrolo [2, 3-B] pyridine as a raw material, carrying out high-selectivity reaction on the 5-fluoro-1H-pyrrolo [2, 3-B] pyridine and a composite chlorination system consisting of phosphorus oxychloride and N, N-dimethylformamide in an aprotic polar solvent under the catalysis of Lewis acid, thereby obtaining the high-purity 4-chloro-5-fluoro-7-azaindole. After the reaction is completed, an integrated quenching-neutralization-extraction post-treatment process is adopted, the operation is simplified, and a crude product is finally recrystallized and purified through a stepped solvent system consisting of ethyl acetate, methyl tert-butyl ether and normal hexane. According to the method, chlorination sites are accurately controlled by optimizing a reaction system, so that by-products are remarkably reduced; meanwhile, the used raw materials and solvents are economical and environment-friendly, and the catalyst is high in efficiency and suitable for industrial production.